Triggered drug release from an antibody-drug conjugate using fast "click-to-release" chemistry in mice

Raffaella Rossin, Sander M.J. van Duijnhoven, Wolter Ten Hoeve, Henk M. Janssen, Laurens H.J. Kleijn, Freek J.M. Hoeben, Ron M. Versteegen, Marc S. Robillard (Corresponding author)

Onderzoeksoutput: Bijdrage aan tijdschriftTijdschriftartikelAcademicpeer review

100 Citaten (Scopus)

Samenvatting

The use of a bioorthogonal reaction for the selective cleavage of tumor-bound antibody-drug conjugates (ADCs) would represent a powerful new tool for ADC therapy, as it would not rely on the currently used intracellular biological activation mechanisms, thereby expanding the scope to noninternalizing cancer targets. Here we report that the recently developed inverse-electron-demand Diels-Alder pyridazine elimination reaction can provoke rapid and self-immolative release of doxorubicin from an ADC in vitro and in tumor-bearing mice.

Originele taal-2Engels
Pagina's (van-tot)1697-1706
Aantal pagina's10
TijdschriftBioconjugate Chemistry
Volume27
Nummer van het tijdschrift7
DOI's
StatusGepubliceerd - 20 jul 2016

Vingerafdruk Duik in de onderzoeksthema's van 'Triggered drug release from an antibody-drug conjugate using fast "click-to-release" chemistry in mice'. Samen vormen ze een unieke vingerafdruk.

Citeer dit